Metoprolol

Metoprolol Brand Names

First-Metoprolol | KAPSPARGO | Lopressor | Toprol XL

What is Metoprolol

Metoprolol is a competitive, beta-1 selective (cardioselective) adrenergic antagonist, which is most similar to atenolol.

It has moderate lipid solubility, lacks intrinsic sympathomimetic activity (ISA), and has weak membrane stabilizing activity (MSA).

Metoprolol is more lipid soluble than atenolol, but less than propranolol and betaxolol. The degree of lipid solubility affects metoprolol’s route of elimination (extensively metabolized) and, theoretically, it’s potential for CNS side effects.

Metoprolol has a relatively short elimination half-life compared to other cardioselective beta-blockers.

It is used for the treatment of hypertension, myocardial infarction, angina, atrial fibrillation or flutter, tremor, migraine, and heart failure.

Cardioselective beta blockers are also utilized in the management of heart failure. The COMET trial evaluated carvedilol vs. metoprolol in patients with chronic heart failure (NYHA Class II—IV), and demonstrated a significantly lower all-cause mortality for carvedilol (34% vs. 40% for metoprolol).

The COMET study has been criticized for utilizing the immediate-release form of metoprolol (tartrate) vs. the extended-release formulation (succinate), which has been FDA-approved for heart failure based on the favorable findings of the MERIT-HF trial.

In the MERIT-HF trial, extended-release metoprolol significantly reduced the incidence of sudden death and mortality due to progressive heart failure in patients receiving conventional therapy (e.g., ACE inhibitors, diuretics, and, in most cases, digitalis).

The COMET trial has also been criticized for evaluating a substantially lower metoprolol target dosage (50 mg PO twice daily) than the FDA-approved target dosage for heart failure (200 mg PO once daily) supported by the MERIT-HF trial.

Authors of the statement also provide recommendations for drug therapy, according to CAD status. In keeping with recent European guidelines, beta-blockers are no longer recommended for blood pressure control in the primary prevention group.

The 2007 AHA guidelines for the management of hypertension state beta-blockers should not be used as first-line therapy for the treatment of hypertension, as several comparative clinical trials have shown beta blockers to be inferior to ACE inhibitors, angiotensin-receptor blockers, or calcium channel blockers for preventing both stroke and coronary artery disease complications.

These guidelines do, however, recommend the use of beta-blockers for the treatment of hypertension in patients with angina, prior myocardial infarction, or heart failure.

The perioperative use of beta blockers to prevent cardiac complications has become somewhat controversial.

In the POISE trial, published online in Lancet in May 2008, 8351 patients with or at risk for atherosclerotic disease were randomized to receive placebo or extended release metoprolol 100 mg 2—4 hours before surgery followed by a daily dose of 200 mg for 30 days following non-cardiac surgery.

Results from this trial show that fewer patients in the extended release metoprolol group had a myocardial infarction compared to the placebo group.

However, the results also indicated that 3.1% of the patients in the extended release metoprolol group died compared with 2.3% in the placebo group, and 1% of patients in the metoprolol group had a stroke compared with 0.5% of those administered placebo.

Metoprolol was initially approved by the FDA in 1978. In February 2001 Toprol-XL™ was approved for the treatment of stable, symptomatic (NYHA Class II—III) heart failure of ischemic, hypertensive, or cardiomyopathic origin, largely based on the MERIT-HF study findings.

Indications

  1. acute myocardial infarction, STEMI
  2. angina
  3. atrial fibrillation
  4. atrial flutter
  5. cardiomyopathy
  6. heart failure
  7. hypertension
  8. migraine prophylaxis
  9. reduction of cardiovascular mortality
  10. tremor
  11. unstable angina

Side Effects

  1. abdominal pain
  2. agranulocytosis
  3. alopecia
  4. amnesia
  5. anxiety
  6. arthralgia
  7. AV block
  8. blurred vision
  9. bradycardia
  10. bronchospasm
  11. chest pain (unspecified)
  12. confusion
  13. constipation
  14. depression
  15. diabetes mellitus
  16. diaphoresis
  17. diarrhea
  18. dizziness
  19. drowsiness
  20. dysgeusia
  21. dyspnea
  22. elevated hepatic enzymes
  23. fatigue
  24. flatulence
  25. hallucinations
  26. headache
  27. heart failure
  28. hepatitis
  29. hyperglycemia
  30. hyperhidrosis
  31. hypertension
  32. hypertriglyceridemia
  33. hypoglycemia
  34. hypotension
  35. impotence (erectile dysfunction)
  36. insomnia
  37. jaundice
  38. laryngospasm
  39. libido decrease
  40. lupus-like symptoms
  41. musculoskeletal pain
  42. nausea
  43. nightmares
  44. palpitations
  45. paresthesias
  46. penile fibrosis
  47. peripheral edema
  48. peripheral vasoconstriction
  49. photosensitivity
  50. pruritus
  51. psoriasis
  52. purpura
  53. pyrosis (heartburn)
  54. rash
  55. retroperitoneal fibrosis
  56. rhinitis
  57. sinus tachycardia
  58. stroke
  59. syncope
  60. thrombocytopenia
  61. thrombotic thrombocytopenic purpura (TTP)
  62. tinnitus
  63. tissue necrosis
  64. tremor
  65. vertigo
  66. visual impairment
  67. vomiting
  68. weight gain
  69. wheezing
  70. withdrawal
  71. xerophthalmia
  72. xerosis
  73. xerostomia

Monitoring Parameters

  • blood pressure
  • heart rate

Contraindications

  • abrupt discontinuation
  • acute bronchospasm
  • acute heart failure
  • asthma
  • AV block
  • beta-blocker hypersensitivity
  • bradycardia
  • breast-feeding
  • bronchitis
  • cardiogenic shock
  • cerebrovascular disease
  • chronic obstructive pulmonary disease (COPD)
  • depression
  • diabetes mellitus
  • driving or operating machinery
  • emphysema
  • geriatric
  • hepatic disease
  • hyperthyroidism
  • hypotension
  • myasthenia gravis
  • peripheral vascular disease
  • pheochromocytoma
  • pregnancy
  • psoriasis
  • pulmonary disease
  • pulmonary edema
  • Raynaud’s phenomenon
  • sick sinus syndrome
  • surgery
  • thyroid disease
  • thyrotoxicosis
  • vasospastic angina
  • ventricular dysfunction

Interactions

  • Abiraterone
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Propoxyphene
  • Adenosine
  • Albiglutide
  • Aldesleukin, IL-2
  • Alemtuzumab
  • Alfentanil
  • Alfuzosin
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Alogliptin; Metformin
  • Alpha-blockers
  • Alpha-glucosidase Inhibitors
  • Alprostadil
  • Amifostine
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amyl Nitrite
  • Antithyroid agents
  • Apomorphine
  • Apraclonidine
  • Aripiprazole
  • Artemether; Lumefantrine
  • Articaine; Epinephrine
  • Asenapine
  • Aspirin, ASA
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Dipyridamole
  • Aspirin, ASA; Omeprazole
  • Aspirin, ASA; Oxycodone
  • Aspirin, ASA; Pravastatin
  • Atazanavir
  • Atazanavir; Cobicistat
  • Baclofen
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Beta-agonists
  • Bismuth Subsalicylate
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bosentan
  • Bretylium
  • Brexpiprazole
  • Bupivacaine
  • Bupivacaine Liposomal
  • Bupivacaine; Lidocaine
  • Bupropion
  • Bupropion; Naltrexone
  • Cabergoline
  • Caffeine; Ergotamine
  • Canagliflozin; Metformin
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Cariprazine
  • Ceritinib
  • Cevimeline
  • Chloroprocaine
  • Chlorthalidone; Clonidine
  • Choline Salicylate; Magnesium Salicylate
  • Cimetidine
  • Cinacalcet
  • Citalopram
  • Clevidipine
  • Clonidine
  • Clozapine
  • Co-Enzyme Q10, Ubiquinone
  • Cobicistat
  • Cocaine
  • Conivaptan
  • Crizotinib
  • Dacomitinib
  • Dapagliflozin; Metformin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Desflurane
  • Desvenlafaxine
  • Dexmedetomidine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Quinidine
  • Diazoxide
  • Digoxin
  • Dihydroergotamine
  • Diltiazem
  • Dipeptidyl Peptidase-4 Inhibitors
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Dipyridamole
  • Disopyramide
  • Donepezil
  • Donepezil; Memantine
  • Doxazosin
  • Dronedarone
  • Dulaglutide
  • Duloxetine
  • Dutasteride; Tamsulosin
  • Eliglustat
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enalapril; Felodipine
  • Encainide
  • Enflurane
  • Epoprostenol
  • Ergonovine
  • Ergotamine
  • Ertugliflozin; Metformin
  • Escitalopram
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Ethanol
  • Etomidate
  • Exenatide
  • Fedratinib
  • Felodipine
  • Fenoldopam
  • Fingolimod
  • Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
  • Flecainide
  • Fluorescein
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluvoxamine
  • food
  • Fospropofol
  • Galantamine
  • General anesthetics
  • Ginger, Zingiber officinale
  • Glipizide; Metformin
  • Glucagon
  • Glyburide; Metformin
  • Guanabenz
  • Guanfacine
  • Haloperidol
  • Halothane
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Icosapent ethyl
  • Iloperidone
  • Iloprost
  • Imatinib
  • Incretin Mimetics
  • Insulin Degludec; Liraglutide
  • Insulin Glargine; Lixisenatide
  • Insulins
  • Intravenous Lipid Emulsions
  • Isocarboxazid
  • Isoflurane
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isosorbide Dinitrate, ISDN
  • Isosorbide Mononitrate
  • Isradipine
  • Ivabradine
  • Ketamine
  • Lacosamide
  • Lanreotide
  • Lasmiditan
  • Levobupivacaine
  • Levodopa
  • Levothyroxine
  • Levothyroxine; Liothyronine (Porcine)
  • Levothyroxine; Liothyronine (Synthetic)
  • Lidocaine
  • Lidocaine; Prilocaine
  • Linagliptin; Metformin
  • Linezolid
  • Liothyronine
  • Liraglutide
  • Lithium
  • Lixisenatide
  • Lofexidine
  • Lopinavir; Ritonavir
  • Lovastatin; Niacin
  • Lurasidone
  • Magnesium Salicylate
  • Mefloquine
  • Meglitinides
  • Mephobarbital
  • Mepivacaine
  • Mepivacaine; Levonordefrin
  • Mestranol; Norethindrone
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methacholine
  • Methohexital
  • Methylergonovine
  • Methysergide
  • Milrinone
  • Mirabegron
  • Nefazodone
  • Nesiritide, BNP
  • Neuromuscular blockers
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicardipine
  • Nifedipine
  • Nimodipine
  • Nisoldipine
  • Nitrates
  • Nitroglycerin
  • Nitroprusside
  • Non-Ionic Contrast Media
  • Nonsteroidal antiinflammatory drugs
  • Octreotide
  • Olanzapine
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oritavancin
  • Oxymetazoline
  • Paliperidone
  • Panobinostat
  • Paroxetine
  • Pasireotide
  • Pentoxifylline
  • Perindopril; Amlodipine
  • Phenelzine
  • Phenothiazines
  • Phenoxybenzamine
  • Phentolamine
  • Pilocarpine
  • Pramlintide
  • Prazosin
  • Prilocaine
  • Prilocaine; Epinephrine
  • Primidone
  • Procainamide
  • Procaine
  • Propafenone
  • Propofol
  • Propoxyphene
  • Quinidine
  • Quinine
  • Ranolazine
  • Rasagiline
  • Remifentanil
  • Reserpine
  • Rifabutin
  • Rifampin
  • Rifamycins
  • Rifapentine
  • Risperidone
  • Ritonavir
  • Rivastigmine
  • Rolapitant
  • Ropivacaine
  • Salsalate
  • Selegiline
  • Semaglutide
  • Sevoflurane
  • SGLT2 Inhibitors
  • Silodosin
  • Siponimod
  • Sufentanil
  • Sulfonylureas
  • Sympathomimetics
  • Tacrine
  • Tamsulosin
  • Tasimelteon
  • Telithromycin
  • Terazosin
  • Terbinafine
  • Tetrabenazine
  • Tetracaine
  • Thalidomide
  • Thiazolidinediones
  • Thiopental
  • Thiothixene
  • Thyroid hormones
  • Tipranavir
  • Tizanidine
  • Trandolapril; Verapamil
  • Tranylcypromine
  • Trazodone
  • Vemurafenib
  • Venlafaxine
  • Verapamil
  • Yohimbine
  • Ziprasidone
You cannot copy content of this page